Intro/Pharmacodynamics

Question 1

Name the percentages and volumes of the following compartments (in males):

1. Total body water
2. ICF
3. ECF (including interstitium and plasma)

Answer 1

1. 60% or 42 L
2. 40% or 28 L
3. ECF: 20% or 14 L
   Interstitium - 10 L
   Plasma - 5% or 3-4 L

Question 2

Do females have more or less total water than males?

Answer 2

Less - 55% compared to males who have 60%

Question 3

Name the AA derivatives of the following:

Dopamine, NE, Epi
Serotonin
Histamine
NO

Answer 3

Tyrosine
Tryptophan
Histidine
Arginine

Question 4

What type of drug is more likely to enter CNS: ionized or lipid soluble?

Answer 4

Lipid soluble

Question 5

Name the general drug targets in order of fastest to slowest action.

Answer 5

Ion channels –> GPCRs –> enzyme-linked receptors –> DNA-linked receptors

Question 6

***statin

Answer 6

HmG-CoA reductase inhibitor, lowers cholesterol, Ex: Lovastatin

Question 7

***pril

Answer 7

ACE inhibitor, lowers BP, Ex: Captopril

Question 8

***navir

Answer 8

HIV protease inhibitor, Ex: Inhinavir

Question 9

***sartan

Answer 9

Angiotensin II receptor blocker, lowers BP, Ex: Losartan

Question 10

***mab

Answer 10

Monoclonal antibody

Question 11

***afil

Answer 11

PDE-5 inhibitor, treats erectile dysfunction and pulmonary hypertension, Ex: Sildenafil (Viagra)

Question 12

***oxin

Answer 12

Cardiac glycoside, Ex: Digoxin

Question 13

***tidine

Answer 13

H2 receptor blocker, reduces stomach acid, Ex: Cimetidine

Question 14

***cillin

Answer 14

Inhibits cell wall synthesis, antibiotic, Ex: Penicillin

Question 15

***cycline

Answer 15

Protein synthesis inhibitor, antibiotic, Ex: Tetracycline

Question 16

What type of drug is capable of producing a maximal effect in the cell or system? What form of R does it bind to?

Answer 16

Full agonist

R’ only - active form

Question 17

What type of drug produces the effect, but not maximally? What form of R does it bind to?

Answer 17

Partial agonist

BOTH R and R’

Question 18

If you increase the concentration of competitive antagonist, what happens to Emax and EC50?

Answer 18

Emax stays the same

EC50 increases

Question 19

If you increase concentration of non-competitive antagonist, what happens to Emax and EC50?

Answer 19

Emax decreases

EC50 stays the same

Question 20

Which type of drug has an effect alone? Antagonist or inverse agonist?

Answer 20

Inverse agonist

Question 21

What form of the receptor do inverse agonists bind to? What effect do they have on activity?

Answer 21

R - inactive form

Decrease activity

Question 22

What type of drug can block the effect of an inverse agonist?

Answer 22

Antagonist

Question 23

True or False. If any receptors are completely knocked out, it is impossible to get the full effect of the drug.

Answer 23

False - spare receptors exist.

Question 24

What term describes the EC50 doses needed to achieve an effect? Would most potent drugs have highest or lowest EC50 value?

Answer 24

Potency - lowest value

Question 25

What term describes the maximal response of drugs? Would most efficacious drugs have highest or lowest Emax values?

Answer 25

Efficacy - highest values

Question 26

What type of drug is Benadryl/Diphenhydramine?

Answer 26

Inverse agonist

Question 27

How do you calculate therapeutic index? What’s more dangerous high index or low?

Answer 27

LD50/ED50

Low

Question 28

Name 5 drugs with low therapeutic index and what they treat.

Answer 28

Theophylin - asthma
Quinine - anti-arrhythmic
Lithium - bipolar
Digoxin - cardiac
Warfarin - anticoagulant